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Facile one-pot four-component synthesis of 3,4-dihydro-2-pyridone derivatives: novel urease inhibitor scaffold.


ABSTRACT: In the current study, a series of 3,4-dihydro-2-pyridone derivatives were synthesized in a one-pot fourcomponent reaction of Meldrum's acid, benzaldehyde derivatives, methyl acetoacetate, and ammonium acetate. SiO2-Pr-SO3H was used as an efficient catalyst for the synthesis of the target compounds under solvent-free conditions. The most probable mechanism for this reaction has been discussed. The advantages of this methodology are high product yields, being environmentally benign, short reaction times, and easy handling. Eight 2-pyridinone derivatives were evaluated for their inhibitory activities against Jack bean urease. Molecular docking study of the synthesized compounds was also evaluated. All compounds showed good activities against urease and among them, 4-(4-nitrophenyl)-5-methoxyc

SUBMITTER: Hakimi AM 

PROVIDER: S-EPMC5615865 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature